A patent review of topoisomerase I inhibitors (2016-present)

Introduction Topoisomerases are important targets for therapeutic improvement in the treatment of some diseases, including cancer. Inhibitors and poisons of topoisomerase I can limit the activity of this enzyme in its enzymatic cycle. This fact implies an anticancer effect of these drugs, since most cancer cells are characterized by both a higher activity of topoisomerase I and a higher replication rate compared to non-cancerous cells. Clinically approved inhibitors include camptothecin (CPT) and its derivatives. However, their limitations have encouraged different research groups to prepare new compounds, proof of which are the numerous research works and patents, some of them in the last five years. Areas covered This review covers patent literature on topoisomerase I inhibitors and their application published between 2016-present. Expert opinion The highest contribution toward patent development has been obtained from academics or small biotechnology companies. The most important fields of innovation include the preparation of prodrugs or inhibitors combined with other agents, as biocompatible polymers or antibodies. A promising development of topoisomerase I inhibitors is expected in the next years, directed to the treatment of diverse diseases, specifically toward different types of cancer and infectious diseases, among others.

Automated summary

Topoisomerase I inhibitors play a crucial role in cancer treatment due to their ability to limit the activity of the enzyme in cancer cells with high replication rates. Clinically approved inhibitors like camptothecin and its derivatives are available, but ongoing research is focused on developing new compounds to address the limitations of existing options. Researchers anticipate promising advancements in the development of topoisomerase I inhibitors, particularly in the treatment of various diseases such as different types of cancer and infectious diseases.